A composition containing oleuropein and/or hydroxytyrosol can be administered to maintain joint health or prevent or treat a joint disorder, for example by preventing or treating cartilage breakdown. The composition can decrease joint pain. An elderly mammal can be the recipient of administration.
Legal claims defining the scope of protection, as filed with the USPTO.
. A method of preventing or treating cartilage breakdown in an individual in need thereof, the method comprising administering an effective amount of oleuropein to the individual.
. The method of, wherein the oleuropein is administered in a composition further comprising an additional component selected from the group consisting of Vitamin D, calcium, phosphorus, magnesium, Vitamin K and mixtures thereof.
. The method of, wherein the oleuropein is the only polyphenol in the composition.
. The method of, wherein the oleuropein is administered in a tablet or capsule.
. The method of, wherein the tablet or capsule further comprises an additional component selected from the group consisting of a cellulosic material, lecithin, and mixtures thereof.
. The method ofwherein the individual is in need of maintained or improved activity and/or mobility.
. The method of, wherein the individual is in need of decreased joint pain.
. The method of, wherein the individual is in need of decreased breakdown of collagen in cartilage.
. The method of, wherein the individual is an elderly mammal.
. The method of, wherein the oleuropein is administered to the individual in a serving of 1 mg to 1 g of the oleuropein.
. The method of, wherein the oleuropein is administered in a composition further comprising at least one additional component selected from the group consisting of antioxidants, anti-inflammatory compounds, glycosaminoglycans, prebiotics, fibres, probiotics, fatty acids, minerals, trace elements and vitamins.
. The method of, wherein the oleuropein is administered in a composition further comprising at least one anti-inflammatory compound.
. The method of, wherein the at least one anti-inflammatory compound is a plant extract.
. The method of, wherein the oleuropein is administered in a composition further comprising at least one antioxidant.
. The method of, wherein the at least one antioxidant is selected from the group consisting of astaxanthin, carotenoids, coenzyme Q10 (“CoQ10″), flavonoids, glutathione, Goji (wolfberry), hesperidin, lactowolfberry, lignan, lutein, lycopene, polyphenols, selenium, vitamin A, vitamin C, vitamin E, and zeaxanthin.
. The method of, wherein the oleuropein is administered in a nutritional composition further comprising at least one of a protein, a carbohydrate or a fat.
. The method of, wherein the oleuropein is administered in a pharmaceutical composition comprising a pharmaceutically acceptable carrier.
. The method of, wherein the oleuropein is administered in a medical food.
. A method of decreasing joint pain in an individual in need thereof, the method comprising administering an effective amount of oleuropein to the individual.
. The method of, wherein the oleuropein is the only polyphenol in the composition.
Complete technical specification and implementation details from the patent document.
This application is a continuation of U.S. application Ser. No. 16/704,211 filed Dec. 5, 2019, which is a continuation-in-part of U.S. application Ser. No. 14/894,602 filed Nov. 30, 2015, which is a National Stage of International Application No. PCT/EP2014/061017 filed May 28, 2014, which claims priority to European Patent Application No. 13169656.9 filed May 29, 2013, the entire contents of which are incorporated herein by reference.
The present invention relates to joint health and in particular to use of a composition comprising oleuropein and/or hydroxytyrosol for prevention or treatment of cartilage breakdown, or maintenance of joint health.
Osteoarthritis (OA) is a high prevalence disease with an important socio-economical impact. It is a degenerative disease of the articular cartilage of the joint, and is the most common form of arthritis, affecting 10% of the adult population. OA is the leading cause of disability in elderly and health care expenses throughout the world.
The progressive breakdown and loss of the articular cartilage belongs to the main features of the pathology, accompanied by changes to other joint structures such as synovial membrane proliferation, sclerosis and thickness of subchondral bone, osteophyte formation at joint margin, ligament laxity and muscle atrophy, all of which contribute to the clinical symptoms of OA. These symptoms include severe pain, stiffness, loss of joint motion and disability.
Although there is an increase of individuals suffering from OA, there is still no cure and current medical therapies remain only palliative, focused on alleviation of symptoms. For example, pain and inflammation are treated using analgesics (such as acetaminophen) and non-steroidal anti-inflammatory drugs (NSAIDs). Furthermore, the use of these drugs is often associated with side effects such as gastrointestinal or cardiovascular risks.
Hence, improved compositions for use in therapy for OA would be advantageous, and in particular more effective and safe compositions are desired.
Anti-inflammatory and antioxidant properties of oleuropein and hydroxytyrosol have been observed previously. However, the inventors have surprisingly demonstrated that these compounds also have anti-catabolic effects on cartilage.
An object of the present invention therefore relates to providing compositions for use in improving joint health. In particular, it is an object of the present invention to provide compositions which improve joint health by preventing or treating cartilage breakdown, and solves the above mentioned problems of the prior art with regards to side effects such as gastrointestinal and/or cardiovascular risks.
Thus, one aspect of the invention relates to a composition comprising oleuropein and/or hydroxytyrosol for use to prevent or treat cartilage breakdown.
Another aspect of the present invention relates to a method of manufacturing a composition for use according to the invention.
Prior to discussing the present invention in further details, the following terms and conventions will first be defined:
In the context of the present invention, mentioned percentages are weight/weight percentages unless otherwise stated.
The term “and/or” used in the context of the “X and/or Y” should be interpreted as “X”, or “Y”, or “X and Y”.
Numerical ranges as used herein are intended to include every number and subset of numbers contained within that range, whether specifically disclosed or not. Further, these numerical ranges should be construed as providing support for a claim directed to any number or subset of numbers in that range. For example, a disclosure of from 1 to 10 should be construed as supporting a range of from 1 to 8, from 3 to 7, from 4 to 9, from 3.6 to 4.6, from 3.5 to 9.9, and so forth.
All references to singular characteristics or limitations of the present invention shall include the corresponding plural characteristic or limitation, and vice versa, unless otherwise specified or clearly implied to the contrary by the context in which the reference is made.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art.
Oleuropein is a polyphenol which has previously been shown to have beneficial effects on inflammation and bone metabolism. Hydroxytyrosol is a related compound, being a metabolite of oleuropein, and has also been shown to have these effects. The inventors have now surprisingly shown that oleuropein and hydroxytyrosol each also have beneficial effects on cartilage breakdown.
Joint disease may be accompanied by inflammation to a greater or lesser degree. In some diseases, the inflammation is an overriding component, such as for example in Rheumatoid arthritis (RA). In other diseases, such as for example OA, the inflammation does not appear as prominently. However, both diseases have a catabolic component in which the articular cartilage is broken down.
The present inventors have shown that the provision of oleuropein can prevent cartilage breakdown in an animal model of OA. Hydroxytyrosol has also been shown to inhibit catabolic enzymes in a cartilage model system.
Thus, the invention in a first aspect relates to a composition comprising Oleuropein and/or hydroxytyrosol for use to prevent or treat cartilage breakdown.
In another manner, this aspect of the invention may be described as the use of oleuropein and/or hydroxytyrosol in the manufacture of a medicament for the prevention or treatment of cartilage breakdown.
The use to prevent or treat cartilage breakdown is synonymous with use to inhibit or decrease cartilage breakdown.
Embodiments of the invention thus include a composition comprising oleuropein for use to prevent or treat cartilage breakdown and a composition comprising hydroxytyrosol for use to prevent or treat cartilage breakdown.
Yet another embodiment of the invention includes a composition comprising Dleuropein and hydroxytyrosol for use to prevent or treat cartilage breakdown.
Further embodiments of the invention include a composition for use according to the invention, wherein the composition further comprises curcumin, as well as a composition for use according to the invention, wherein the composition further comprises quercetin.
In embodiments of the invention the composition for use according to the invention comprises oleuropein and/or hydroxytyrosol, as well as one or more further polyphenol, for example one or more further polyphenols selected from the group consisting of curcumin, and quercetin.
One embodiment of the invention relates to a composition for use according to the invention, wherein the composition comprises oleuropein and/or hydroxytyrosol and further comprises curcumin.
The combination of oleuropein and curcumin, as well as the combination of hydroxytyrosol and curcumin, have both been shown to inhibit catabolic enzymes in an in vitro model of cartilage (see, Example 1).
Another embodiment of the invention relates to a composition for use according to the invention, wherein the composition comprises oleuropein and/or hydroxytyrosol and further comprises quercetin.
The combination of oleuropein and quercetin, as well as the combination of hydroxytyrosol and quercetin, have both been shown to inhibit catabolic enzymes in an in vitro model of cartilage (see, Example 1).
In yet another embodiment, the composition for use according to the invention comprises oleuropein and/or hydroxytyrosol, and further comprises curcumin and quercetin.
The combinations of oleuropein+curcumin+quercetin, or hydroxytyrosol+curcumin+quercetin, have each been shown to have synergistic and specific effects on the catabolic enzymes active in cartilage breakdown (see, Example 1).
The oleuropein, hydroxytyrosol, curcumin and quercetin are the main bioactive molecules according to present invention. They may be from any suitable source. In preferred embodiments, oleuropein, hydroxytyrosol, curcumin and quercetin are obtained from plant sources. Oleuropein and hydroxytyrosol may for example be obtained from the olive plant.
The compositions for use according to the invention may also comprise at least one further bioactive compound, such as a compound selected from the group consisting of antioxidants, anti-inflammatory compounds, glycosaminoglycans, prebiotics, fibres, probiotics, fatty acids, minerals, trace elements and/or vitamins.
The term “bioactive” in the context of the present application means that the compound contributes to the health of an individual, or has an effect on the human body, beyond that of meeting basic nutritional need.
The at least one further bioactive compound may be from a natural source. Thus the compounds may be from extracts of plants, animals, fish, fungi, algae, microbial fermentation. Minerals are considered as from natural source also within this definition.
Anti-Inflammatory Compounds and/or AntioxidantsCombination with Anti-Inflammatory Compounds
The present invention relates in one aspect to compositions for use to prevent or treat cartilage breakdown.
In one embodiment of the invention, the compositions according to the invention are for combined use with at least one anti-inflammatory compound.
The at least one anti-inflammatory compound may be administered in combination with a composition of the invention, for example sequentially or simultaneously.
The at least one anti-inflammatory compound may be provided in the same composition as the composition of the invention, or may be provided in separate compositions, for example in a kit of parts, or a series of interacting products.
If the composition for use according to the invention and the at least one anti-inflammatory compound are presented in one or more separate compositions, they may be mixed prior to administration, or may be administered simultaneously or sequentially.
In further embodiments, the composition for use according to the invention comprises at least one anti-inflammatory compound as an at least one further bioactive compound. In other preferred embodiments, the composition for use according to the invention comprises at least one antioxidant as an at least one a further bioactive compound.
The at least one anti-inflammatory and/or antioxidant compound may be any suitable compound with anti-inflammatory and/or antioxidant effect.
It is noted that several anti-inflammatory compounds also have antioxidant effect. A compound may be selected for inclusion based on it having either or both properties.
Examples of anti-inflammatory compounds which may be included in a composition of the invention are anti-inflammatory compounds from natural sources.
Thus, one embodiment of the invention relates to a composition for use according to the invention, wherein the at least one anti-inflammatory compound comprises omega-3 polyunsaturated fatty acids, which may for example be extracted from fish.
Other embodiments of the invention relate to compositions for use according to the invention, wherein the at least one anti-inflammatory compound comprised is at least one plant extract.
The plant extract may comprise for example flavonoids, polyphenols, proanthocyanins, lipids (such as avocado soybean unsaponifiables, omega-3 polyunsaturated fatty acids).
Plant extracts may be from one or more plants selected from the group consisting of devil's claw (),, hyssop, ginger (), turmeric (),, willow bark, pomegranate (Punica granatum), green tea (), cat's claw (Uncaria tometosa and Uncaria guianensis), Indian olibaum (), and pineapple bromelain (), Black seed (Nigella), St. John's wort, hyperforin, Goldenseal, German Chamomile ().
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October 23, 2025
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